pparγ lbd

Leriglitazone, a metabolite of pioglitazone, binds to the PPARγ C-terminal ligand-binding domain (Ki: 1.2 μM) and induces transcriptional efficacy of the PPARγ (EC50: 680 nM). Leriglitazone PioOH is a PPARγ agonist, stabilizes the PPARγ activation functio

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

PPARγmodulator-2 (Compound (R)-2n) is a reversible modulator of PPARγ, inhibiting the PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. It helps lower blood glucose levels, improves glucose tolerance and insulin sensitivity, and demonstrates antidiabetic activity in db db mouse models.

Leriglitazone (Hydroxypioglitazone) hydrochloride, a pioglitazone metabolite, acts as a PPARγ agonist, effectively stabilizing the PPARγ activation function-2 (AF-2) co-activator binding surface to enhance co-activator binding, which results in a modest improvement in transcriptional efficacy. It binds to the PPARγ C-terminal ligand-binding domain (LBD) with a dissociation constant (K i) of 1.2 μM and demonstrates transcriptional efficacy with an effective concentration (EC 50) of 680 nM [1].